Publication
Title
Antileishmanial activity of a series of -disubstituted quinazoline-2,4-diamines
Author
Abstract
A series of N-2,N-4-disubstituted quinazoline-2,4-diamines has been synthesized and tested against Leishmania donovani and L. amazonensis intracellular amastigotes. A structure-activity and structure-property relationship study was conducted in part using the Topliss operational scheme to identify new lead compounds. This study led to the identification of quinazolines with EC50 values in the single digit micromolar or high nanomolar range in addition to favorable physicochemical properties. Quinazoline 23 also displayed efficacy in a murine model of visceral leishmaniasis, reducing liver parasitemia by 37% when given by the intraperitoneal route at 15 mg kg(-1) day(-1) for 5 consecutive days. Their antileishmanial efficacy, ease of synthesis, and favorable physicochemical properties make the N-2,N-4-disubstituted quinazoline-2,4-diamine compound series a suitable platform for future development of antileishmanial agents.
Language
English
Source (journal)
Journal of medicinal chemistry. - Washington, D.C., 1963, currens
Publication
Washington, D.C. : 2014
ISSN
0022-2623
Volume/pages
57:12(2014), p. 5141-5156
ISI
000338184100012
Full text (Publisher's DOI)
Full text (publisher's version - intranet only)
UAntwerpen
Faculty/Department
Research group
[E?say:metaLocaldata.cgzprojectinf]
New tools for monitoring drug resistance and treatment response in visceral leishmaniasis in the Indian subcontinent. (KALADRUG-R)
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 08.09.2014
Last edited 13.11.2017
To cite this reference